卵巢癌是最致命的妇科癌症。溴结构域和额外末端结构域 (BET) 蛋白在表观遗传水平的基因表达调控中发挥着重要作用。 Jun Qi (JQ1) 是 BET 蛋白的有效抑制剂。鉴于半衰期短和药代动力学较差，JQ1 被装载到新开发的纳米载体中。壳聚糖纳米粒子是癌症治疗中最好且最有潜力的聚合物之一。本研究旨在构建壳聚糖-JQl纳米颗粒（Ch-J-NPs），用Ch-J-NPs处理OVCAR-3细胞，并评估这些纳米颗粒对细胞周期和凋亡相关基因的影响。纳米粒子的合成和表征。 Ch-J-NP 的尺寸和形态通过 DLS 和 FE-SEM 技术确定。培养 OVCAR-3 细胞并用 Ch-J-NP 处理。然后，使用MTT测定法测量IC50。定义组并用 IC50 浓度的 Ch-J-NP 处理细胞 48 小时。最后，使用定量 RT-PCR 评估不同组细胞中目的基因的表达。Ch-J-NP 的 IC50 值为 5.625 μg/mL。 RT-PCR 结果表明，用 Ch-J-NP 处理癌细胞后，与细胞周期活性相关的基因（c-MYC、hTERT、CDK1、CDK4 和 CDK6）的表达显着降低。相反，caspase-3和caspase-9的表达显着增加。 Ch-J-NPs处理细胞后，BAX（促凋亡）与BCL2（抗凋亡）表达比也显着增加。Ch-J-NPs对OVCAR-3细胞表现出显着的抗细胞周期和凋亡作用。版权所有：© 2024 药物科学研究。

Ovarian cancer is the deadliest gynecological cancer. Bromodomain and extra terminal domain (BET) proteins play major roles in the regulation of gene expression at the epigenetic level. Jun Qi (JQ1) is a potent inhibitor of BET proteins. Regarding the short half-life and poor pharmacokinetic profile, JQ1 was loaded into newly developed nano-carriers. Chitosan nanoparticles are one of the best and potential polymers in cancer treatment. The present study aimed to build chitosan-JQl nanoparticles (Ch-J-NPs), treat OVCAR-3 cells with Ch-J-NPs, and evaluate the effects of these nanoparticles on cell cycle and apoptosis-associated genes.Ch-J-NPs were synthesized and characterized. The size and morphology of Ch-J-NPs were defined by DLS and FE-SEM techniques. OVCAR-3 cells were cultured and treated with Ch-J-NPs. Then, IC50 was measured using MTT assay. The groups were defined and cells were treated with IC50 concentration of Ch-J-NPs, for 48 h. Finally, cells in different groups were assessed for the expression of genes of interest using quantitative RT-PCR.IC50 values for Ch-J-NPs were 5.625 μg/mL. RT-PCR results demonstrated that the expression of genes associated with cell cycle activity (c-MYC, hTERT, CDK1, CDK4, and CDK6) was significantly decreased following treatment of cancer cells with Ch-J-NPs. Conversely, the expression of caspase-3, and caspase-9 significantly increased. BAX (pro-apoptotic) to BCL2 (anti-apoptotic) expression ratio, also increased significantly after treatment of cells with Ch-J-NPs.Ch-J-NPs showed significant anti-cell cyclic and apoptotic effects on OVCAR-3 cells.Copyright: © 2024 Research in Pharmaceutical Sciences.